Asc-241 U0126

Biological Description

selective non-competitive inhibitor of MAP kinase kinase (MKK). Inhibits MKK1, MKK2 (IC₅₀ values of 0.07 and 0.06 μM respectively) and MKK5 with little or no effect on a wide range of other kinases. Centrally active following systemic administration in vivo.

Useful References

Favata et al (1998) Identification of a novel inhibitor of mitogen-activated protein kinase kinase. J Biol Chem. 273:18623-32 abstract



Duncia et al (1998) MEK inhibitors: the chemistry and biological activity of U0126, its analogs, and cyclization products. Bioorg Med Chem Lett. 8:2839-44 abstract



Bain et al (2007)The selectivity of protein kinase inhibitors: a further update. Biochem J. 408:297-315 abstract

 

Chemical Information

1,4-Diamino-2,3-dicyano-1,4-bis(2-aminophenylthio)butadiene

• Desiccate at +4°C


• MW 380.49


• Soluble to 100 mM in DMSO


• C₁₈H₁₆N₆S₂


• 109511-58-2